珊瑚菌菌体培养物的新天然产物 （英文稿）

目的 对珊瑚菌(Clavicorona pyxidata)菌体培养物的活性成分进行分离。方法 用多种色谱技术对化合物进行分离纯化,并用光谱技术和单晶X射线衍射技术鉴定化合物的结构。结果 从中分离到2个化合物: clavicoronol(1)、腺苷(2)。结论 化合物1为新化合物,并通过单晶X射线衍射技术确定了2的立体构型。     

乳香中一个新的甘遂烷型三萜

为研究乳香的化学成分,本文采用硅胶柱色谱和高效液相色谱从乳香95%乙醇浸膏中分离得到2个化合物,通过IR、UV、NMR和HR-ESI-MS等方法对其进行结构解析,并借助ECD计算确定其绝对构型,分别是:7α-羟基-3,11-二羰基-甘遂-8,24-二烯-21-酸(1)和21β-羟基-3-乙酰基-11-羰基-β-乳香酸(2),其中化合物1是新化合物,化合物2为首次采用ECD计算确定其绝对构型的已知化合物。     

腺梗豨莶中一个新二萜类化合物的分离与结构解析(英文)

从腺梗豨莶中分离得到一个新的ent-pimarane型二萜类化合物ent-16-nor-3-oxo-pimar-8(14)-en-15-al(1),以及4个已知二萜类化合物kirenol(2),ent-2-oxo-15,16,19-trihydroxypimar-8(14)-ene(3),darutigenol(4),darutoside(5)。化合物1的平面结构及相对构型通过波谱学方法确定。     

牛膝中牛膝甾酮25位异构体构型的确定及其抗肿瘤活性的研究

目的牛膝 (AchyranthesbidentataBl.)中牛膝甾酮 2 5位异构体的分离、鉴定、构型确定以及肿瘤抑制活性的测定。方法利用硅胶吸附柱色谱和HPLC法进行分离 ,利用理化性质和波谱分析对化合物进行鉴定 ;利用体外实验法测定其活性。结果 2个非对映异构体化合物分别鉴定为 2 5 R牛膝甾酮 (2 5 Rinokosterone ,1)和 2 5 S牛膝甾酮 (2 5 Sinokosteone ,2 )。化合物 1具有一定的肿瘤抑制活性。结论 2个化合物均为首次从牛膝中分离得到 ,首次确定了其绝对构型 ,并首次对牛膝甾酮 2个 2 5位异构体进行了1H NMR、13 C NMR数据归属。牛膝中发挥肿瘤抑制作用的成分主要应为皂苷类成分。     

花刺柳珊瑚共生真菌Penicillium sp. gx wz406的次生代谢产物研究

目的从珊瑚共生真菌中获得抗肿瘤药物先导化合物。方法通过集成化学与细胞毒性的筛选方法筛选目标菌株,采用现代色谱和波谱的方法分离鉴定目标菌株的活性代谢产物,通过化学沟通鉴定化合物的绝对立体构型。结果和结论从采自广西涠洲岛的花刺柳珊瑚(Echinogorgia floraNutting)中筛选获得了1株具有细胞毒活性的青霉菌(Penicillium sp.)gxwz406,从其发酵产物中分离鉴定了5个化合物:S(-)-2-(2-hydroxypropanamido)benzamide(1)、R(+)-chrysogine(2)2、-pyruvylaminobenzamide(3)、nicotinamide(4)和2',3'-dihydrosorbicillin(5),并首次确定了化合物1的绝对构型。     

垫状卷柏中一个新的炔酚类衍生物(英文)

采用硅胶、Sephadex LH-20等多种材料进行分离纯化,通过理化方法和波谱分析进行结构鉴定,从垫状卷柏全草中分离并鉴定了两个炔酚类衍生物,分别为selaginellin S(1)和M(2)。其中,化合物1为新炔酚类衍生物,是炔酚类成分生源合成途径的关键前体物质;通过ECD计算确定了其绝对构型。化合物2为首次从该植物中报道。     

鹧鸪花果实trichilin-type柠檬苦素化学成分研究

通过常压硅胶、凝胶、反相柱色谱和高压反相柱色谱等色谱技术对楝科植物鹧鸪花果实的化学成分进行研究,从鹧鸪花(Trichilia connaroides)果实乙醇提取物中分离获得4个trichilin-type柠檬苦素,包括2个新化合物和2个已知化合物3α-deacetylamoorastatin (3)和mesendanins K (4)。通过综合运用HR-ESI-MS、1H NMR、13C NMR、HSQC、HMBC和ROESY等多种光谱分析方法确定了新化合物1、2的平面结构和相对构型。通过对分离获得的化合物进行肿瘤细胞毒活性研究,结果表明新化合物1、2和已知化合物4对宫颈癌细胞(HeLa)具有微弱的细胞毒活性。     

从红树林内生真菌Penicillium sp. SCNU-F0003中分到的一个新的tetronic acid二聚体

目的 为了评价从红树林内生真菌Penicillium sp. SCNU-F0003中分离得到的新化合物(+)-(5R, 5?R)-3,3?-methylenebistetronic acid (1)和5个已知化合物的潜在活性。方法 通过核磁数据分析和单晶衍射分析确定化合物1的绝对构型,并测定所有化合物的抗氧化活性和α-葡萄糖苷酶抑制活性。结果 化合物1显示中等抗氧化活性,IC50值为81.6 μM,化合物2显示出α-葡萄糖苷酶抑制活性,比阳性药物阿卡波糖 (IC50 = 725.1 μM) 活性更好。结论 化合物1 和2具有潜在的生物活性。     

圆二色谱在单萜和木脂体化合物结构分析中的应用

报道了10个化合物的CD谱,其中栀子酮(1)、栀二醇(2)和木脂体(3～7)均为新化合物。应用5种规则,确定了它们的绝对构型。     

一株南极来源真菌Arthrinium arundinis的次级代谢产物研究

目的 对一株南极海泥来源真菌Arthrinium arundinis (FNJ20) 的次级代谢产物进行研究。方法 运用硅胶柱层析、Sephadex LH-20凝胶柱层析和半制备HPLC等方法对A. arundinis (FNJ20)的大米发酵提取物进行分离纯化;通过NMR及MS等波谱学方法进行结构解析,通过X-ray单晶衍射实验确定化合物的绝对构型,并测定化合物的抗细菌及真菌活性。结果 从A. arundinis (FNJ20)的大米发酵提取物中分离鉴定出6个二萜类化合物（1–6）及2个苯并色原酮类化合物（7–8）,首次获得化合物1的单晶数据,并确证其绝对构型与文献相反。抗菌活性评价结果表明,化合物8具有对金黄色葡萄球菌和白色念珠菌具有显著的抑制活性,其MIC值分别为6.25和12.50 μM。     

Synthesis and anti-inflammatory activity of alkyl/arylidene-2-aminobenzothiazoles and 1-benzothiazol-2-yl-3-chloro-4-substituted-azetidin-2-ones

Ten new derivatives of 1-benzothiazol-2-yl-3-chloro-4-substituted-azetidin-2-ones (3a-j) were synthesized using various Schiff bases (alkyl/arylidene-2-aminobenzothiazoles; 2a-j), which in turn were prepared starting from 2-aminobenzothiazole (1). All the synthesised compounds were characterised by elemental analyses and spectral (IR, 1H-NMR, 13C-NMR and EI-MS) data. The title compounds 2a-j and 3a-j were screened in vivo using carrageenan-induced rat paw edema model. All the test compounds showed anti-inflammatory activity when tested in vivo. In general, compounds 3a-j were found to be more potent compared to compounds 2a-j. Among the compounds tested, compound 2g in the alkyl/arylidene-2-aminobenzothiazoles series and compound 3 g in the 1-benzothiazol-2-yl-3-chloro-4-substituted-azetidin-2-ones series were found to be the most potent. All the test compounds were also evaluated to check the gastric ulcer incidence. In gastric ulceration studies, all the test compounds were generally found to be safe at the 100 mg/kg dose level. Furthermore the most potent compounds 2 g and 3 g from each series were screened in vitro for inhibition of both COX-2 and COX-1 catalysed prostaglandin biosynthesis (radiochemical assay). Like most of the commercially available non-steroidal anti-inflammatory drugs (NSAIDs), in the in vitro study, compounds 2 g and 3 g showed anti-inflammatory activity by blocking the metabolism of arachidonic acid to prostaglandin via the cyclooxygenase pathways. In general, in the vitro assay, test compounds 2 g and 3 g were found to be more active after 15 min pre-incubation with the enzyme. Compound 3 g was found to be more COX-2 selective, while compound 2 g was found to be equally COX-2 and COX-1 selective.     

Inhibitory effects of acylated kaempferol glycosides from the leaves of Cinnamomum kotoense on the proliferation of human peripheral blood mononuclear cells

A new chemical entity, namely kaempferol 3- O-alpha-L-[2-(Z)-p-coumaroyl-4-(E)-p-coumaroyl]rhamnopyranoside (1), and the known kaempferol 3-O-alpha-L-[2,4-di-(E)-p-coumaroyl]rhamnopyranoside (2) have been isolated from the methanolic extract of leaves of Cinnamomum kotoense. Structural elucidation of compounds 1 and 2 were achieved on the basis of spectroscopic analysis. The effects of compounds 1 and 2 on phytohemagglutinin (PHA) stimulated cell proliferation were studied towards human peripheral blood mononuclear cells (PBMC). The results indicated that compounds 1 and 2 suppressed PBMC proliferation induced by PHA with an IC50 value of 5.0 +/- 1.3 and 6.0 +/- 1.5 microM, respectively. Interleukin-2 production in activated PBMC inhibited by compounds 1 and 2 were in a concentration-dependent manner. Therefore, we suggested that compounds 1 and 2 in C. kotoense were likely the growth modulators for PBMC.     

Synthesis and anticonvulsant activity of a new series of 1,4-dihydropyridine derivatives

A series of 1,4-dihydropyridine derivatives (1a-g) were prepared from three compounds condensation of Hantzsch synthesis. A new series of 2,2'-{[4-(aryl)-2,6-dimethyl-1,4-dihydropyridine-3,5-diyl]dicarbonyl}dihydrazinecarbothioamide (2a-g) were prepared from compounds diethyl 4-(aryl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate (1a-g) reacted with thiosemicarbazide to give the corresponding compounds (2a-g) by hydrazinolysis method. The synthesized compounds were confirmed by IR, (1)HNMR, (13)CNMR, mass spectral and elemental analyses. The newly synthesized compounds (2a-g) were screened for anticonvulsant activity against in swiss albino rat. The test was evaluated by maximal electrode induced convulsion method. Synthesized compounds were used two (50 and 100 mg/kg) concentrations. Compounds (1a-g) were inactive while compounds (2a-g) have moderate anti-convulsant activity compared with standard phenytoin drug. The compound 2,2'-{[4-(furan-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-diyl]dicarbonyl} dihydrazinecarbothioamide (2a) has highly active compared with other compound (2b-2g).     

Chemical constituents from the Moutan Cortex charcoal and their potential coagulation activities

The chemical constituents of Cortex Moutan charcoal were studied in depth, and their coagulation activity was screened. The chemical constituents were isolated by polyamide, silica gel and Sephadex G-Sepharose chromatography purification,and their structures were identified by NMR spectroscopy and other analyses. A total of 10 compounds were obtained and identified as follows: 3-(2-furan)-1-(2-hydroxy-4-methoxy-phenyl)-2-propylene ketone (1), 2-(2,5-hydroxy-4-methyl phenyl) propionate ethyl ester (2), methyl tetradec-5-enoate (3), 1,4-diethylcyclohexane (4), catechol (5), methyl-4-hydroxybenzoate (6), 3-hydroxy-2-methyl-4-pyrone (7), 3,8-dihydroxy-2-metyl-chromone (8), 3β-hydroxy-olean-12-en (9), 1-monolinolein (10). Among them, compounds 1 and 2 were new natural products, and 3–10 were isolated from the Cortex Moutan charcoal for the first time. The potential coagulation activities of compounds were evaluated, and compounds 2, 9 and 10had strong hemostatic effects. While compounds 1 and 8 could significantly activate blood circulation.     

2-[5-取代苯并咪(噻)唑-2-硫基]-1-(4-取代苯基)乙酮缩氨基胍的合成及NHE1抑制活性

目的设计合成缩氨基胍类化合物并研究其NHE1抑制活性。方法以4-取代苯乙酮(1)为原料,经溴代得α-溴代物(2),再与2-巯基-5-取代苯并咪(噻)唑(3)反应得到2-(5-取代苯并咪(噻)唑-2-硫基)-1-(4-取代苯基)乙酮(4),最后与氨基胍缩合得到目标化合物;以血小板肿胀模型进行初步的体外NHE1抑制活性筛选。结果与结论合成了12个新化合物,其结构经IR、1H-NMR及MS确证。初步的药理试验表明,12个目标化合物均有一定的NHE1抑制活性,其中化合物5b和5h的活性明显优于阳性对照药卡立泊来德。     

苯烷基异硫脲类化合物的合成及其一氧化氮合酶抑制活性苯烷基异硫脲类化合物的合成及其一氧化氮合酶抑制活性

目的寻找抑制神经型一氧化氮合酶(nNOS)并对痴呆症等有较好治疗作用的化合物。方法以异硫脲为母核,在其结构中引入苯烷基得到目的物,通过药物对神经细胞中亚硝酸盐含量的影响，测定目的物对nNOS的抑制作用。结果设计合成了16个新的苯烷基异硫脲类化合物(I1～16)。其结构经MS,IR,¹HNMR和元素分析确证。所有目的物均有不同程度的nNOS抑制活性，其中化合物I₈,I₁₂和I₁₄的活性较强。结论化合物I₈,I₁₂和I₁₄的活性强于阳性对照药S-甲基-N-(4-甲氧基苯基)异硫脲,IC₅₀达到1×10-7 mol·L^-1水平。     

A STUDY IN MICE OF BROMO AND CHLORO ACYLUREA ANALOGUES OF THE SEDATIVE-HYPNOTIC BROMUREIDES

1. A series of 1-(2-chloroacyl)ureas, related to the sedative-hypnotic drugs brom-valetone and carbromal, was synthesized and tested in mice to determine central depressant and acute toxic effects. Four 1-(2-bromoacyl)ureas and two 3-halo compounds were included for comparison. 2. Large variations in potency were seen between the compounds. Much of this can be ascribed to differences in lipophilicity. Among homologous 1-(2-chloroacyl)ureas, those with 6 acyl carbons had maximal potency. Among groups of structural isomers, the most potent were 2-halo, 3-alkyl substituted compounds. 3. The most potent compounds were also those with the largest ratios of hypnotic to lethal activity. 4. The variation in the onset and duration of action of these compounds enables a choice to be made for a compound with a particular set of characteristics.     

5-氨基-6,8-二氟-1-(5-氟-2-吡啶基)-7-(3-甲基-1-哌嗪基)-1,4-二氢-4-氧代喹啉-3-羧酸及其类似物的合成及其抗菌作用

目的设计合成1-位为5-氟-2-吡啶基的吡酮酸衍生物,并对其抗菌活性进行初步评价.方法以2,3,4,5-四氟-6-硝基苯甲酰基乙酸乙酯和2,4,5-三氟-3-甲氧基苯甲酰基乙酸乙酯为原料,经多步反应合成8个5-氨基-6,8-二氟-1-(5-氟-2-吡啶基)-7-(3-甲基-1-哌嗪基)-1,4-二氢-4-氧代喹啉-3-羧酸及其类似物.结果共合成15个新化合物,经¹HNMR和MS确证其结构,其中8个(8-15)为目标物.结论8个目标物对金黄色葡萄球菌-16、大肠埃希氏菌-26和铜绿假单孢菌-17的体外活性均低于环丙沙星.     

Ferulates, amurenlactone A and amurenamide A from traditional Chinese medicine cortex Phellodendri Amurensis

Two new ferulate compounds, amurenlactone A (1) and amurenamide A (2), along with 11 known compounds have been isolated from the cortex of Phellodendron amurense. The structures of the new compounds were established based on 1D, 2D NMR and mass spectral analyzes. The known compounds were identified by comparison with authentic samples.     

1-[2-(取代苯基甲硫基)-2-(2,4-二氟苯基)乙基]-1H-1,2,4-三唑类化合物的合成及抗真菌活性

设计合成了21个1-[2-(取代苯基甲硫基)-2-(2,4-二氟苯基)乙基]-1H-1,2,4-三唑类化合物,其中19个为首次报道。体外抑菌试验表明:所有目标化合物对8种试验真菌均有不同程度的抗菌活性,其中化合物1,2,5对絮状表皮癣菌的活性为硫康唑的512倍以上;化合物5对白色念株菌的活性为硫康唑的32倍;化合物2对申克孢子丝菌的活性为硫康唑的32倍;化合物2,14对新型隐球菌的活性分别为硫康唑的64倍,32倍;化合物1,5对熏烟色曲菌的活性分别为硫康唑的16倍以上。